ArticlesPilocarpine Prodrugs II. Synthesis, Stability, Bioconversion, and Physicochemical Properties of Sequentially Labile Pilocarpine Acid Diesters
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Prodrugs - Current development and applications in ocular drug delivery
2021, Journal of Drug Delivery Science and TechnologyCitation Excerpt :Pilocarpine is a cholinergic agent commonly used to treat or manage glaucoma. It has a lower absorption in the cornea, therefore it cannot penetrate into the ocular tissues as its log P is −0.15 [63]. Design and synthesis of pilocarpine prodrug (Fig. 5) in ocular drug delivery has proven beneficial and improves the corneal absorption of the parent drug.
Ocular prodrugs: Attributes and challenges
2021, Asian Journal of Pharmaceutical SciencesCitation Excerpt :It exhibits low level of absorption in the corneal site due to which it cannot penetrate into ocular tissues to exhibit its effect. Its log P value is −0.15 [102]. So the answer to the above problem was in the synthesis of pilocarpine prodrug (Fig. 10) that would improve the corneal absorption of parent drug and prove beneficial in ocular drug delivery.
Prodrugs incorporated into nanotechnology-based drug delivery systems for possible improvement in bioavailability of ocular drugs delivery
2013, Asian Journal of Pharmaceutical SciencesCitation Excerpt :Although some lipophilic prodrugs present a promising ocular absorption, their highly lipophilic nature leads them to be difficult to dissolve in an aqueous medium, and raises a challenge in drug delivery in the form of eyedrops, in which form more than 90% of marketed ophthalmic formulations are developed. Such situations are exemplified by O-palmitoyl timolol [54] and pilocarpic acid diesters [53]. In the case of O-palmitoyl timolol, the prodrugs were administered in rabbits as a dispersion, because of low aqueous solubility, which may produce poor patient compliance and hinder their further use clinically.
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